[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide
TPCA-1 Pale yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable ureidocarboxamido thiophene compound that acts as a potent inhibitor of IKK-2 (IC50 = 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-a production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Further reduces paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg). Purity: ≥95% by HPLC. CAS 507475-17-4. Ref.: Podolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373. Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17. Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4. |
